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Method for preparing tricarbonyl technetium-99m intermediate

a tricarbonyl intermediate and tricarbonyl technology, applied in the field of tricarbonyl tricarbonyl intermediate preparation, can solve the problems of affecting the clinical application of the above-mentioned methods, affecting the clinical application of the hospital, and the routine application of the clinical practice is not feasible, so as to achieve easy operation, high labeling yield, and easy to obtain raw materials

Active Publication Date: 2020-01-09
INST OF HIGH ENERGY PHYSICS CHINESE ACADEMY OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

This patent describes a method for making technetium-99m tricarbonyl, which is a key intermediate in the production of various technetium-labeled probes. The method is simple, uses easily obtained raw materials, and has a high labeling yield. This technique can be used to create a variety of technetium tricarbonyl labeled probes.

Problems solved by technology

At early stage, the technetium tricarbonyl complex is usually synthesized at high temperature and high pressure through a multi-step reaction, which is not feasible for the routine application in clinical practice.
However, the methods above-mentioned each has defects, for example, the use of gaseous CO, the complicated preparation of K2[H3BCO2], the labeling under condition of heating, etc.
These defects hinder their clinical application and promotion in hospital.

Method used

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  • Method for preparing tricarbonyl technetium-99m intermediate
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  • Method for preparing tricarbonyl technetium-99m intermediate

Examples

Experimental program
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Effect test

example 1

[0068]The technetium tricarbonyl intermediate was prepared by using cyclopentadienyl manganese tricarbonyl as the carbon monoxide source and sodium borohydride as the reducing agent.

[0069]200 mg of cyclopentadienyl manganese tricarbonyl, 10 mg of sodium borohydride, 20 mg of potassium sodium tartrate, and 4 mg of sodium carbonate were weighed and added to a quartz bottle before the addition of 1 mL (37 MBq) freshly prepared 99mTcO4− eluent. After being shaken greatly, the quartz bottle was sealed and placed under a hand-held UV lamp (254 nm) with a reaction proceeding for 20 min at room temperature. After the reaction, the mixture obtained was adjusted to a pH of 6 to 7 by 0.1 mol / L hydrochloric acid and filtered by a syringe to obtain the product technetium tricarbonyl intermediate [99mTc(H2O)3(CO)3]+. HPLC analysis revealed the product peak with a retention time of 9.2 min and a labeling yield of 96%.

example 2

[0070]The technetium tricarbonyl intermediate was prepared by using methyl cyclopentadienyl manganese tricarbonyl as the carbon monoxide source and sodium borohydride as the reducing agent.

[0071]20 mg of methyl cyclopentadienyl manganese tricarbonyl, 5.5 mg of sodium borohydride, 20 mg of potassium sodium tartrate, and 4 mg of sodium carbonate were weighed and added to a penicillin bottle before the addition of 1 mL (37 MBq) freshly prepared 99mTcO4− eluent. After being shaken greatly, the penicillin bottle was sealed and placed under a hand-held UV lamp (365 nm) with a reaction proceeding for 20 min at room temperature. After the reaction, the mixture obtained was adjusted to a pH of 6 to 7 by 0.1 mol / L hydrochloric acid and filtered by a syringe to obtain the product technetium tricarbonyl intermediate [99mTc(H2O)3(CO)3]+. HPLC analysis revealed the product peak with a retention time of 9.5 min and a labeling yield of 98%, and the chromatograms was shown in FIG. 1.

example 3

Preparation of Cyclopentadienecarboxylic Acid Manganese Tricarbonyl

[0072]

[0073]1 g of cyclopentadienyl manganese tricarbonyl was weighed and dissolved in 10 mL anhydrous tetrahydrofuran. A solution of N-butyl lithium in hexane (3.37 mL, 1.6 mol / L) was dropwise added to the tetrahydrofuran solution under the protection of −45° C. argon. After the dropwise addition, excess dry ice was added to obtain a mixture which was stirred at room temperature for 2 h. After the reaction, the solvent was evaporated under reduced pressure, and then water and ethyl acetate were added to the mixture obtained with being shaken greatly. Hydrochloric acid was added to the water phase to produce precipitate which was collected and dried obtaining 0.76 g yellow powder (cyclopentadienecarboxylic acid manganese tricarbonyl) with a yield of 62.5%.

Preparation of the Technetium Tricarbonyl Intermediate [99mTc(H2O)3(CO)3]+

[0074]The technetium tricarbonyl intermediate was prepared by using cyclopentadienecarboxy...

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Abstract

The invention provides a method for preparing a technetium-99m tricarbonyl intermediate. The method comprises reacting a manganese carbonyl compound used as a carbon monoxide source with pertechnetate and water to obtain the technetium-99m tricarbonyl intermediate. The method for preparing a technetium-99m tricarbonyl intermediate in an embodiment of the invention can complete the preparation of the intermediate at atmospheric pressure and room temperature. The method is easy to operate, uses easily obtained raw materials, has a high labeling yield, and can be used to prepare various types of technetium tricarbonyl labeled probes.

Description

TECHNICAL FIELD[0001]The present invention relates to a method for preparing technetium-99m tricarbonyl intermediate, and particularly, to a method for preparing technetium-99m tricarbonyl intermediate at atmospheric pressure and room temperature.BACKGROUND[0002]By means of Molecular Imaging, a molecular process under normal or pathological state can be studied by way of non-invasive imaging technology. The molecular imaging diagnostic method in nuclear medicine, which comprises single photon emission computed tomography (SPECT) and positron emission tomography (PET), has been widely applied in clinical practice. It has a high specificity and a high sensitivity, and is therefore an important direction for the molecular imaging research.[0003]The radionuclide technetium-99m (99mTc), as a good nuclide with characteristics of low cost, simple preparation, low radioactive dose and multi-valence, is well known as an excellent nuclide for SPECT. Among the monovalent metal technetium radio...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): C07F17/00
CPCC07F17/00C01G99/00C07F13/00C01P2002/87C07B59/004
Inventor YANG, WENJIANGLIU, YUXUE, JINGQUANZHANG, YANHUA
Owner INST OF HIGH ENERGY PHYSICS CHINESE ACADEMY OF SCI
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